title: Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
abstract: From the X-ray crystal structures of linezolid and the non-selective antibiotic sparsomycin, we have derived a new family of hybrid oxazolidinones. From this initial compound set we have developed a new biaryloxazolidinone scaffold that shows both potent antimicrobial activity as well as selective inhibition of ribosomal translation. The synthesis of these compounds is outlined.
authors.affiliation: Department of Medicinal Chemistry, Rib-X Pharmaceuticals Inc., 300 George Street, Suite 301, New Haven, CT 06511, USA.
authors.forename: Jiacheng
authors.initials: J
authors.lastname: Zhou
authors.forename: Ashoke
authors.initials: A
authors.lastname: Bhattacharjee
authors.forename: Shili
authors.initials: S
authors.lastname: Chen
authors.forename: Yi
authors.initials: Y
authors.lastname: Chen
authors.forename: Erin
authors.initials: E
authors.lastname: Duffy
authors.forename: Jay
authors.initials: J
authors.lastname: Farmer
authors.forename: Joel
authors.initials: J
authors.lastname: Goldberg
authors.forename: Roger
authors.initials: R
authors.lastname: Hanselmann
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Ippolito
authors.forename: Rongliang
authors.initials: R
authors.lastname: Lou
authors.forename: Alia
authors.initials: A
authors.lastname: Orbin
authors.forename: Ayomi
authors.initials: A
authors.lastname: Oyelere
authors.forename: Joe
authors.initials: J
authors.lastname: Salvino
authors.forename: Dane
authors.initials: D
authors.lastname: Springer
authors.forename: Jennifer
authors.initials: J
authors.lastname: Tran
authors.forename: Deping
authors.initials: D
authors.lastname: Wang
authors.forename: Yusheng
authors.initials: Y
authors.lastname: Wu
authors.forename: Graham
authors.initials: G
authors.lastname: Johnson
mesh_terms: D000081:Acetamides / Q000494:pharmacology; D000284:Administration, Oral; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004926:Escherichia coli / Q000187:drug effects; D006193:Haemophilus influenzae / Q000187:drug effects; D000069349:Linezolid; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure; D001936:Moraxella catarrhalis / Q000187:drug effects; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014176:Protein Biosynthesis / Q000187:drug effects; D013033:Sparsomycin / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D013033:Sparsomycin; D000069349:Linezolid